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. Author manuscript; available in PMC: 2010 Feb 22.
Published in final edited form as: Annu Rev Pharmacol Toxicol. 2007;47:731–759. doi: 10.1146/annurev.pharmtox.47.120505.105134

Table 1.

Endothelin receptor antagonists used in experimental studies of Pulmonary Arterial Hypertension

Drug Selectivity ETAKi ETBKi Orally
active
(yes/no)		 Models investigated Effect
(+) beneficial
(o) no effect
(−) harmful		 Investigator, Year
RO 47-0203 ETA & ETB 4.7 nM 95 nM Yes Overcirculation + Rondelet, 2003
(Bosentan) Monocrotaline + Hill, 1997
Hypoxia + Holm, 1996
Hypoxia + Chen, 1995
Vascular Study McCulloch, 1998
SB217242 ETA 1.1 nM 111 nM Yes Hypoxia + Underwood, 1998
(Enrasentan) Hypoxia + Underwood, 1997
Hypoxia + Underwood, 1999
Vascular Study MacLean, 1998
SB234551 ETA 0.1 nM 500 nM Yes Vascular Study MacLean, 1998
SB209670 ETA & ETB 0.2 nM 12 nM No Vascular Study McCulloch, 1998
Vascular Study MacLean, 1998
BSF420627 ETA & ETB 2.2 nM 5.8 nM Yes Monocrotaline + Jasmin, 2001
BQ123 ETA 22 nM 18 µM No Overcirculation + Ivy, 1997
Hypoxia + DiCarlo, 1995
Hypoxia + Oparil, 1995
Hypoxia + Bonvallet, 1994
Monocrotaline + Miyauchi, 1993
BQ-610 ETA 0.7 nM 24 µM No Hypoxia + Ambalavanan, 2005
Hypoxia + Ambalavanan, 2002
EMD122946 ETA 0.032 nM 160 nM No Hypoxia + Ambalavanan, 2002
TBC3711 ETA 0.08 nM 26.3 µM Yes Hypoxia + Perreault, 2001
TBC11251 ETA 1.4 nM 9.8 µM Yes Monocrotaline + Tilton, 2000
(Sitaxsentan)
TA-0201 ETA 0.015 nM 41 nM Yes Monocrotaline + Ueno, 2000
Monocrotaline + Ueno, 2002
BMS-193884 ETA 1.4 nM 18.8 µM Yes Monocrotaline + Miyauchi, 2000
ZD1611 ETA 8.6 nM 5.6 µM Yes Hypoxia + Bialecki, 1999
Hypoxia + Bialecki, 1998
FR 139317 ETA 1 nM 7 µM No Vascular Study McCulloch, 1998
ABT-627 ETA 0.034 nM 63.3 nM Yes Monocrotaline + Nishida, 2004
(Atrasentan) Monocrotaline + Nishida, 2004
BMS 182874 ETA 55 nM >200 µM Yes Vascular Study McCulloch, 1998
YM598 ETA 0.697 nM 569 nM Yes Hypoxia + Yuyama, 2005
Monocrotaline + Yuyama, 2004
Monocrotaline + Fujimori, 2004
LU135252 ETA 1.4 nM 140 nM Yes Monocrotaline + Jasmin, 2003
(Darusentan) Monocrotaline + Jasmin, 2001
Monocrotaline + Prie, 1998
Monocrotaline + Prie, 1997
Hypoxia + Blumberg, 2003
PD-155080 ETA 221.4 nM 86.5 µM Yes Monocrotaline + Stessel, 2004
PD-156707 ETA 0.17 nM 133.8 nM Yes Overcirculation + Fratz, 2004
Hypoxia + Sheedy, 1998
Hypoxia + Haleen, 1998
Vascular Study Black, 2003